| Size | Price | Stock | Qty |
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| 25mg |
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Bavdegalutamide (ARV110; ARV-110) is an orally bioavailable PROTAC-based Androgen Receptor (AR) degrader with potential anticancer activity. May be used for the treatment of metastatic castration-resistant prostate cancer (mCRPC).
| ln Vitro |
In all examined cell lines, bavdegalutamide totally destroys AR, with a 50% degradation concentration (DC50) of less than 1 nM [1]. In LNCaP cells, bavdegalutamide (0.01 nM-300 nM) degrades AR in a dose-dependent manner [1]. The degradation of AR in VCaP cells is caused in a time-dependent manner by bavdegalutamide (10 nM; 0.5-24 hours) [2]. At low nanomolar doses, bavdegalutamide (10-1000 nM) causes apoptosis, suppresses AR-dependent cell growth, and inhibits the production of the AR target gene PSA [2]. In the hyperandrogenic milieu of VCaP cells (R1881, 100 nM), bavdegalutamide (0.01 nM-100 nM) degrades clinically relevant mutant AR proteins (WT AR, F876L, T877A, M896V, and H874V) while maintaining its activity [2].
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| ln Vivo |
Bavdegalutamide (oral gavage; 1 mg/kg; QD) displays better than 90% breakdown of AR in vivo. Bavdegalutamide also revealed strong inhibitory effects on tumor growth and AR signaling in LNCaP, VCaP, and prostate cancer patient-derived xenograft (PDX) models [2]. Bavdegalutamide (oral gavage; 3 or 10 mpk; 30 days) demonstrated in vivo effectiveness and decrease in AR target gene expression in a long-term, castrated, enzalutamide-resistant VCaP tumor model. The TGIs for the 3 mpk and 10 mpk dosages were 70% and 60%, respectively. respectively[2].
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| References |
[1]. Taavi Neklesa, et al. ARV-110: An androgen receptor PROTAC degrader for prostate cancer. American Association for Cancer Research. 2018. 78 (13): pp. 5236.
[2]. Taavi K Neklesa,et al. ARV-110: an oral androgen receptor PROTAC degrader for prostate cancer. GU ASCO 2019 |
| Molecular Formula |
C41H43CLFN9O6
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|---|---|
| Molecular Weight |
812.2882
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| CAS # |
2222112-77-6
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| SMILES |
ClC1=C(C#N)C([H])=C([H])C(=C1[H])OC1([H])C([H])([H])C([H])([H])C([H])(C([H])([H])C1([H])[H])N([H])C(C1C([H])=C([H])C(=NN=1)N1C([H])([H])C([H])([H])C([H])(C([H])([H])C1([H])[H])C([H])([H])N1C([H])([H])C([H])([H])N(C2=C(C([H])=C3C(N(C(C3=C2[H])=O)C2([H])C(N([H])C(C([H])([H])C2([H])[H])=O)=O)=O)F)C([H])([H])C1([H])[H])=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~26.67 mg/mL (~32.83 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.79 mg/mL (0.97 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.9 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 10 mg/mL (12.31 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication (<60°C). Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2311 mL | 6.1554 mL | 12.3109 mL | |
| 5 mM | 0.2462 mL | 1.2311 mL | 2.4622 mL | |
| 10 mM | 0.1231 mL | 0.6155 mL | 1.2311 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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